UCI-LC0019
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer.
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- Purity: 98.63%
- CAS No.: 1372406-51-3
- 화학식: C17H14N2O2
- 분자량:278.31
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| HCT-116 | IC50 |
0.58 μM
Compound: A9
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Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
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[PMID: 27017265] |
UCI-LC0019 potently inhibits proliferation of p53G245S-expressing Saos-2 cells (IC50 = 16.5 μM) and p53R175H-expressing TOV112D cells (IC50 = 15.2 μM) with reduced activity against p53null Saos-2 cells (IC50 = 24.1 μM)[1].
UCI-LC0019 (0-30 μM; 3-72 h) rapidly reduces proliferation and induces apoptosis in p53R175H-expressing TOV112D cells[1].
UCI-LC0019 (25-30 μM; 3 days) inhibits proliferation of p53R175H-expressing TOV112D cells via a mechanism independent of thiol reactivity, as co-treatment with 5 mM NAC (HY-B0215) does not reverse its antiproliferative effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:p53R175H-expressing TOV112D cells
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Concentration:30 μM
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Incubation Time:3, 12, 24 h
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Result:Induced rapid cell death time-dependently.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with p53R175H-expressing TOV112D Xenografts[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily for 10 days
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Result:Reduced tumor volume.
Increased GSH levels.
Did not result in weight loss or any obvious toxic effects.
Chemical Information
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CAS No. 1372406-51-3
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Appearance Solid
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분자량 278.31
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화학식 C17H14N2O2
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Color Light yellow to yellow
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SMILES
COC1=CC=CC(/C=C/C(C2=NC3=CC=CC=C3N2)=O)=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
순도&문서
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Data Sheet (271 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
UCI-LC0019 Related Classifications
HY-186151 Related Classifications
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